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Assay Detail

CHEMBL763404

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Binding
Inhibitory activity against HIV protease
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Human immunodeficiency virus type 1 protease (CHEMBL243) ↗
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Preparation and structure-activity relationship of novel P1/P1'-substituted cyclic urea-based human immunodeficiency virus type-1 protease inhibitors.
Nugiel DA, Jacobs K, Kaltenbach RF, Worley T, Patel M, Meyer DT, Jadhav PK, De Lucca GV, Smyser TE, Klabe RM, Bacheler LT, Rayner MM, Seitz SP.
J Med Chem (1996) 39 : 2156 -2169
PubMed 8667359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 47 7.89 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL433497 — — 1 9.96
CHEMBL444047 — — 1 9.62
CHEMBL21145 DMP-323 — 1 9.57
CHEMBL308694 — — 1 9.36
CHEMBL431762 — — 1 9.33
CHEMBL68904 — — 1 9.06
CHEMBL73225 — — 1 8.96
CHEMBL305228 — — 1 8.96
CHEMBL431702 — — 1 8.89
CHEMBL431306 — — 1 8.72
CHEMBL68086 — — 1 8.60
CHEMBL421488 — — 1 8.60
CHEMBL70210 — — 1 8.57
CHEMBL443792 — — 1 8.55
CHEMBL70041 — — 1 8.54
CHEMBL290576 — — 1 8.47
CHEMBL303625 — — 1 8.47
CHEMBL303035 — — 1 8.37
CHEMBL302585 — — 1 8.37
CHEMBL304327 — — 1 8.33
CHEMBL262503 — — 1 8.32
CHEMBL303422 — — 1 8.24
CHEMBL552674 — — 1 8.15
CHEMBL66007 — — 1 8.08
CHEMBL68317 — — 1 8.07
CHEMBL308649 — — 1 8.07
CHEMBL67813 — — 1 8.04
CHEMBL262387 — — 1 8.01
CHEMBL69746 — — 1 7.89
CHEMBL304153 — — 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL433497 — Ki = 0.11 nM 9.96
CHEMBL444047 — Ki = 0.24 nM 9.62
CHEMBL21145 DMP-323 Ki = 0.27 nM 9.57
CHEMBL308694 — Ki = 0.44 nM 9.36
CHEMBL431762 — Ki = 0.47 nM 9.33
CHEMBL68904 — Ki = 0.87 nM 9.06
CHEMBL73225 — Ki = 1.1 nM 8.96
CHEMBL305228 — Ki = 1.1 nM 8.96
CHEMBL431702 — Ki = 1.3 nM 8.89
CHEMBL431306 — Ki = 1.9 nM 8.72
CHEMBL68086 — Ki = 2.5 nM 8.60
CHEMBL421488 — Ki = 2.5 nM 8.60
CHEMBL70210 — Ki = 2.7 nM 8.57
CHEMBL443792 — Ki = 2.8 nM 8.55
CHEMBL70041 — Ki = 2.9 nM 8.54
CHEMBL290576 — Ki = 3.4 nM 8.47
CHEMBL303625 — Ki = 3.4 nM 8.47
CHEMBL303035 — Ki = 4.3 nM 8.37
CHEMBL302585 — Ki = 4.3 nM 8.37
CHEMBL304327 — Ki = 4.7 nM 8.33
CHEMBL262503 — Ki = 4.8 nM 8.32
CHEMBL303422 — Ki = 5.8 nM 8.24
CHEMBL552674 — Ki = 7.1 nM 8.15
CHEMBL66007 — Ki = 8.4 nM 8.08
CHEMBL308649 — Ki = 8.5 nM 8.07
CHEMBL68317 — Ki = 8.6 nM 8.07
CHEMBL67813 — Ki = 9.1 nM 8.04
CHEMBL262387 — Ki = 9.8 nM 8.01
CHEMBL69746 — Ki = 13.0 nM 7.89
CHEMBL304153 — Ki = 22.0 nM 7.66
CHEMBL69632 — Ki = 28.0 nM 7.55
CHEMBL308695 — Ki = 32.0 nM 7.50
CHEMBL68793 — Ki = 35.0 nM 7.46
CHEMBL69743 — Ki = 38.0 nM 7.42
CHEMBL303151 — Ki = 46.0 nM 7.34
CHEMBL304108 — Ki = 60.0 nM 7.22
CHEMBL304520 — Ki = 65.0 nM 7.19
CHEMBL433293 — Ki = 86.0 nM 7.07
CHEMBL431552 — Ki = 160.0 nM 6.80
CHEMBL433123 — Ki = 250.0 nM 6.60
CHEMBL69731 — Ki = 320.0 nM 6.50
CHEMBL69457 — Ki = 580.0 nM 6.24
CHEMBL71447 — Ki = 1100.0 nM 5.96
CHEMBL306194 — Ki = 1700.0 nM 5.77
CHEMBL70056 — Ki = 2500.0 nM 5.60
CHEMBL66817 — Ki = 3900.0 nM 5.41
CHEMBL432336 — Ki = 5000.0 nM 5.30